С целью поиска новых противосудорожных субстанций синтезирован ряд 2-(4-оксо-2-тиоксо-1H-хиназолин-3-ил)ацетамидов взаимодействием 4-оксо-2-тиоксо-1,4-дигидрохиназолин-3(2H)-ил)уксусной кислоты с соответствующими аминами в присутствии N,N’-карбонилдиимидазола. На модели пентилентетразоловых судорог у мышей исследуемые вещества показали слабый и умеренный противосудорожный эффект. Обсуждены некоторые закономерности «структура — активность».
Aegopodium podagraria is used as a sedative in trad itional medicine. The effect of its aerial part ext ract and tincture on levels of depression and anxiety, as we ll as on locomotor activity, exploratory behaviour and memory of male and female mice was investigated. The extract showed dose-dependent and sex specific antidepressi ve effect (at a dose of 100 mg/kg but not at a dose of 1 g/kg in female mice) with the worsening of the results of the passive avoidance test. The extract at a dose of 100 mg/kg tended to reduce anxiety signs in the animals of b oth sexes , in male mice such reduction was also seen under the in fluence of the extract at a dose of 1 g/kg and the tincture at doses of 1 and 5 ml/kg (the latter did not consider ably changed the other parameters measured). The re sults indicate favourable central activity of A. podagraria extrac t in mice.
The new compound, 2-methyl-3-phenylaminomethylquinolin-4-on, belongs to V class of toxicity and exhibits antidepressant and antiamnesic properties. It is established that this compound reduces the duration of immobilization in the test of behavioral despair, prevents from the scopolamine induced amnesia, and exhibits antagonism with reserpine in mice. In a dose of 100 mg/kg, the synthesized compound influences the levels of cerebral catecholamines similarly to imipramine, but with a more pronounced decrease in the level of 5-hydroxytryptamine.
The review summarizes verified data on the medicinal plants of world flora that influence the kidney excretory function. The biologically active substances of herbal preparations, the mechanisms of the renal effects, and the accompanying pharmacological properties of nephrotropic plants are considered.
Experiments on rats showed that the increased use of NaCl modulates the renal activity of enalapril. In animals with a model edema syndrome caused by subdiaphragm constriction of the interior vena cava, a hyper-NaCl diet enhances the Na-diuretic action of enalapril in both subacute and chronic stage of circulation insufficiency. In addition, enalapril increases the creatinin secretion in rats with this model (but not in intact animals). The administraton of enalapril in animals with caval obstruction receiving excess NaCl, in contrast to the case of standard diet, decreases the consumption of water, thus preventing the development of a positive balance of water.
The stimulating effect of curiozin gel and plaster application on the engraftment of skin autografts from various areas of body was studied in rats. Curiozin gel in a single dose of 75 mg was used for the daily treatment of autografts over the entire postoperation period of time. The adhesive plaster was applied onto skin autografts for 5 days after skin transplantation. The skin autografts in the test group exhibited normalized volume blood flow dynamics, reduced duration of the inflammatory reaction, and improved the quality of engraftment as compared to the untreated control group. The best healing and blood-flow-normalizing effect was achieved by combined application of curiozin gel and adhesive plaster.